WO2018139885A1 - Composition comprising acetoxychavicol acetate as active ingredient for preventing hair loss and promoting hair growth - Google Patents
Composition comprising acetoxychavicol acetate as active ingredient for preventing hair loss and promoting hair growth Download PDFInfo
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- WO2018139885A1 WO2018139885A1 PCT/KR2018/001141 KR2018001141W WO2018139885A1 WO 2018139885 A1 WO2018139885 A1 WO 2018139885A1 KR 2018001141 W KR2018001141 W KR 2018001141W WO 2018139885 A1 WO2018139885 A1 WO 2018139885A1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
- A61K31/222—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/37—Esters of carboxylic acids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q7/00—Preparations for affecting hair growth
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
- A23V2200/318—Foods, ingredients or supplements having a functional effect on health having an effect on skin health and hair or coat
Definitions
- the present invention relates to a composition for preventing hair loss or promoting hair growth comprising acetoxychavicol acetate as an active ingredient.
- the present invention relates to a pharmaceutical composition, a quasi-drug composition, a cosmetic composition, and a food composition for preventing hair loss or promoting hair growth comprising acetoxychabicol acetate as an active ingredient.
- Hair loss refers to a condition in which there is no hair in the area where hair should normally exist, and generally means that the hair of the scalp (coarse hair) falls out.
- Hair loss is a disease that occurs not only by aging but also by many factors in combination with young age. Specifically, the cause of hair loss may include internal factors such as genetic constitution and the action of testosterone, external stress such as daily stress, dietary habits, and accumulation of lipid peroxide in the scalp.
- hair loss in young people including obesity hair loss in women as well as male hair loss has been gradually spread, and many kinds of hair loss treatment agents, hair growth agents, etc. are commercially available to improve the hair loss phenomenon.
- Minoxidil (minoxidil), a typical anti-hair loss treatment on the market, was originally developed for the treatment of hypertension, but it is a drug that has become more famous as a hair regrowth agent due to side effects of use.
- minoxidil preparations are known to cause side effects such as contact dermatitis or hirsutism, such as scalp pruritus, erythema, and keratin overuse (J Korean Med Assoc 2013 January; 56 (1): 45-54).
- Propesia blocks the 5-alpha-reductase type 2 enzyme, which plays an important role in the development of androgenetic alopecia, thereby inhibiting the change of testosterone to dihydrotestosterone (DHT). It is known to improve or inhibit the progression of hair loss. Propecia is known to have excellent hair loss prevention effects, but the reagents used to manufacture it are expensive and toxic, and because it acts in a way that artificially blocks the production of steroid hormones itself, many side effects may occur. There is a danger. Therefore, there is still a need for the development of a safe treatment agent having excellent efficacy of preventing hair loss and promoting hair growth, but having no side effects.
- DHT dihydrotestosterone
- An object of the present invention is to provide a composition for preventing hair loss or promoting hair growth comprising acetoxychavicol acetate (acetoxychavicol acetate) as an active ingredient.
- an object of the present invention is to provide a pharmaceutical composition for preventing hair loss or promoting hair growth, quasi-drug composition, cosmetic composition and food composition comprising acetoxychabicol acetate as an active ingredient.
- the present invention provides a pharmaceutical composition for preventing hair loss or promoting hair growth comprising acetoxychavicol acetate (acetoxychavicol acetate) or a pharmaceutically acceptable salt thereof as an active ingredient.
- the compound of Formula 1 may be chemically synthesized or separated from natural materials, and may be purchased and used commercially at home and abroad.
- the type of plant is not particularly limited, but may be separated using a root diameter of Alpinia galanga . It is also possible to prepare plant extracts containing a high concentration of acetoxychabicol acetate.
- the present inventors can prepare a high extract of acetoxychabicol acetate using the root of the mass steel ( Alpinia galanga, Thailand).
- the root of the mass steel Alpinia galanga, Thailand.
- 250 ml of 70% aqueous ethanol was added and the ultrasonic extraction was repeated twice for 2 hours.
- the filtrate was concentrated under reduced pressure at 40 °C ⁇ 50 °C, and then lyophilized to give 2.2 g (yield 4.4%) of 70% ethanol extract of the mass root diameter.
- the acetoxychabicol acetate content in the obtained extract was found to be 14.61% (FIG. 3).
- the compound of formula 1 of the present invention has the effect of promoting the growth of hair follicles.
- human hair follicle cells (n 36) divided into four groups, the first group is a control (control) not treated with the drug, the second group is treated with testosterone 500 nM, the third group In the test group treated with 500 nM of silver testosterone and 100 nM of acetoxycarbicol acetate and 200 nM of testosterone and 200 nM of acetoxycarbicol acetate, hair follicles in the test group treated only with testosterone had a small size. While showing a reduction of more than 40%, both experimental groups treated with testosterone and acetoxychabicol acetate were confirmed to maintain the size of the hair follicles to a similar degree as the control group not treated with testosterone (FIG. 2). This demonstrates that the reduction in hair follicle size and thus hair growth inhibition by testosterone is restored by acetoxychabicol acetate.
- the compound of formula 1 of the present invention has the effect of inhibiting the production of free radicals (ROS) in skin cells.
- ROS free radicals
- the compound of formula 1 of the present invention has the effect of inhibiting the activity of NADPH oxidase (Nox) in skin cells.
- the present invention also provides a pharmaceutical composition for the prevention or treatment of hair loss comprising acetoxychavicol acetate (acetoxychavicol acetate) or a pharmaceutically acceptable salt thereof as an active ingredient as a compound represented by the following formula (1).
- salts in a form that can be used pharmaceutically among salts in which cations and anions are bound by electrostatic attraction, and are generally metal salts and organic bases. Salts with, inorganic acids, salts with organic acids, salts with basic or acidic amino acids, and the like.
- the metal salt may be an alkali metal salt (sodium salt, potassium salt, etc.), alkaline earth metal salt (calcium salt, magnesium salt, barium salt, etc.), aluminum salt, or the like;
- Salts with organic bases include triethylamine, pyridine, picoline, 2,6-lutidine, ethanolamine, diethanolamine, triethanolamine, cyclohexylamine, dicyclohexylamine, N, N-dibenzylethylenediamine Salts and the like;
- Salts with inorganic acids can be salts with hydrochloric acid, hydrobromic acid, nitric acid, sulfuric acid, phosphoric acid, and the like;
- Salts with organic acids can be salts with formic acid, acetic acid, trifluoroacetic acid, phthalic acid, fumaric acid, oxalic acid, tartaric acid, maleic acid, citric acid, succinic acid, methanesulfonic acid, benzenesulf
- the pharmaceutical composition of the present invention may further include a pharmaceutically acceptable carrier in addition to including the compound of formula 1 or a pharmaceutically acceptable salt thereof as an active ingredient.
- the type of the carrier is not particularly limited, and any carrier may be used as long as it is commonly used in the art.
- Non-limiting examples of the carrier include saline, sterile water, Ringer's solution, buffered saline, albumin injection solution, lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, maltodextrin, glycerol, ethanol, and the like. Can be. These may be used alone or in combination of two or more thereof.
- composition of the present invention may be used, if necessary, by adding other pharmaceutically acceptable additives such as excipients, diluents, antioxidants, buffers or bacteriostatic agents, fillers, extenders, wetting agents, disintegrants, dispersants, surfactants , Binders or lubricants may be additionally added and used.
- other pharmaceutically acceptable additives such as excipients, diluents, antioxidants, buffers or bacteriostatic agents, fillers, extenders, wetting agents, disintegrants, dispersants, surfactants , Binders or lubricants may be additionally added and used.
- the compound of Formula 1 or a pharmaceutically acceptable salt thereof may be included in an amount of 0.00001% to 99.99% by weight based on the total weight of the pharmaceutical composition, preferably 1% by weight. % To 99.99% by weight, more preferably 10% to 99.99% by weight, more preferably 50% to 99.99% by weight, and may also be included in the total content of the pharmaceutical composition.
- compositions of the present invention can be formulated and used in a variety of formulations suitable for oral or parenteral administration.
- Non-limiting examples of the formulation for oral administration include troches, lozenges, tablets, aqueous suspensions, oily suspensions, prepared powders, granules, emulsions, hard capsules, soft capsules, syrups or elixirs, and the like. Can be mentioned.
- a binder such as lactose, saccharose, sorbitol, mannitol, starch, amylopectin, cellulose or gelatin and the like; Excipients such as dicalcium phosphate and the like; Disintegrants such as corn starch or sweet potato starch; Lubricants such as magnesium stearate, calcium stearate, sodium stearyl fumarate or polyethylene glycol wax and the like can be used, and sweeteners, fragrances, syrups and the like can also be used.
- a liquid carrier such as fatty oil may be additionally used in addition to the above-mentioned materials.
- Non-limiting examples of the parenteral preparations include injection liquids, suppositories, respiratory inhalation powders, spray aerosols, ointments, application powders, oils, creams, and the like.
- a sterile aqueous solution In order to formulate the pharmaceutical composition for parenteral administration, a sterile aqueous solution, a non-aqueous solvent, a suspension, an emulsion, a freeze-dried preparation, an external preparation, and the like may be used.
- the non-aqueous solvent and the suspension may be propylene glycol, Polyethyleneglycol, vegetable oils such as olive oil, injectable esters such as ethyloleate and the like can be used.
- the composition of the present invention When formulating the pharmaceutical composition of the present invention into an injection solution, the composition of the present invention is mixed in water with a stabilizer or buffer to prepare a solution or suspension which is formulated for unit administration of ampoules or vials. can do.
- a propellant or the like may be combined with the additive to disperse the dispersed dispersion or the wet powder.
- a cream, a powder for application an oil, an external skin preparation, etc., animal oil, vegetable oil, wax, paraffin, starch, tracant, cellulose derivative, polyethylene glycol, silicone, bentonite , Silica, talc, zinc oxide and the like can be formulated using a carrier.
- compositions of the present invention may vary depending on the formulation method, mode of administration, time of administration and / or route of administration of the pharmaceutical composition, and the reaction to be achieved by the administration of the pharmaceutical composition.
- the type and extent of the subject type, age, weight, general state of health, condition and extent of the disease, sex, diet, excretion, and components of the drug or other composition used concurrently or simultaneously with the subject. And various similar factors well known in the medical arts, and those skilled in the art can readily determine and prescribe a dosage effective for the desired treatment.
- Administration of the pharmaceutical composition of the present invention may be administered once a day, may be divided into several times.
- the pharmaceutical compositions of the present invention may be administered as individual therapeutic agents or in combination with other therapeutic agents and may be administered sequentially or simultaneously with conventional therapeutic agents. All of the above factors can be considered and administered in an amount that can obtain the maximum effect in a minimum amount without side effects, which can be easily determined by those skilled in the art.
- the route of administration and mode of administration of the pharmaceutical compositions of the present invention may be independent of each other, and may be any route of administration and mode of administration without particular limitation, so long as the pharmaceutical composition can reach the desired site of interest.
- the pharmaceutical composition may be administered by oral or parenteral administration.
- intravenous administration intraperitoneal administration
- intramuscular administration intramuscular administration
- transdermal administration or subcutaneous administration may be used, and the method of applying, spraying or inhaling the composition to a diseased site may also be used, but the present invention is not limited thereto. It doesn't work.
- the pharmaceutical composition of the present invention may be preferably used in a method of directly applying or spreading on hair, skin or scalp.
- hair may include all parts of the hair root and hair follicles throughout the body, such as hair roots and hair follicles of hair, hair, eyelashes, eyelashes, and beards.
- the present invention provides a quasi-drug composition for preventing hair loss or promoting hair growth comprising acetoxychabicol acetate, or a pharmaceutically acceptable salt thereof, as a compound represented by the following Formula 1.
- quasi-drugs exclude products used for the purpose of medicines, and include products used for the treatment or prevention of diseases of humans and animals, and products with slight or no direct action on the human body.
- the compound of Formula 1 of the present invention when used as an quasi-drug additive, it may be added as it is or used with other quasi-drug or quasi-drug components, and may be appropriately used according to a conventional method.
- the mixing ratio with other ingredients used together may be suitably determined depending on the purpose of use (eg, prevention, improvement or therapeutic treatment).
- Examples of the quasi-drug composition may include, but are not limited to, scalp hair care compositions such as shampoos and rinses, body cleansers, foams, soaps, masks, ointments, creams, lotions, essences, sprays, and the like.
- scalp hair care compositions such as shampoos and rinses, body cleansers, foams, soaps, masks, ointments, creams, lotions, essences, sprays, and the like.
- the quasi-drug composition comprising the compound of formula 1 of the present invention or a pharmaceutically acceptable salt thereof as an active ingredient may preferably be a composition for scalp hair care.
- composition for scalp hair care refers to a composition that prevents or alleviates damage to the scalp and hair.
- the formulation of the scalp hair care composition may be, but is not limited to, shampoo, rinse, essence, nutrient, serum, massage cream, lotion, pack, and the like.
- the compound of Formula 1 or a pharmaceutically acceptable salt thereof may be included in an amount of about 0.001 to 50% by weight, preferably about 10% by weight, based on the total weight of the quasi-drug composition.
- the present invention provides a cosmetic composition for preventing hair loss or promoting hair growth comprising acetoxychabicol acetate or a cosmetically acceptable salt thereof as an active ingredient, which is a compound represented by Formula 1 below.
- cosmetically acceptable salts refers to salts that can be used cosmetically even among salts in which cations and anions are bonded by electrostatic attraction. Specific examples include examples of the "pharmaceutically acceptable salts" described above.
- Formulation of the cosmetic composition of the present invention is, for example, solution, shampoo, rinse, external ointment, cream, foam, nourishing lotion, flexible lotion, pack, flexible water, latex, makeup base, essence, liquid cleanser, bath, sun Screen creams, sun oils, suspensions, emulsions, pastes, gels, lotions, powders, soaps, surfactant-containing cleansing, oils, powder foundations, emulsion foundations, wax foundations, patches, sprays, and the like. Do not.
- the cosmetic composition of the present invention may further include one or more cosmetically acceptable carriers formulated in general cosmetics, and as common components, for example, oil, water, surfactants, moisturizers, lower alcohols, thickeners, Chelating agents, pigments, preservatives, fragrances and the like can be appropriately blended, but is not limited thereto.
- one or more cosmetically acceptable carriers formulated in general cosmetics, and as common components, for example, oil, water, surfactants, moisturizers, lower alcohols, thickeners, Chelating agents, pigments, preservatives, fragrances and the like can be appropriately blended, but is not limited thereto.
- the cosmetically acceptable carrier included in the cosmetic composition of the present invention may vary depending on the formulation of the cosmetic composition.
- the carrier component is animal oil, vegetable oil, wax, paraffin, starch, tragacanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc, zinc oxide Etc. may be used, but is not limited thereto. These may be used alone or in combination of two or more thereof.
- lactose, talc, silica, aluminum hydroxide, calcium silicate, polyamide powder, and the like can be used, in particular, in the case of a spray, additionally chlorofluorohydrocarbons.
- Propellant such as, but not limited to, propane / butane or dimethyl ether. These may be used alone or in combination of two or more thereof.
- a solvent, solubilizer or emulsion may be used as the carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, Propylene glycol, 1,3-butylglycol oil, and the like can be used, and in particular, cottonseed oil, peanut oil, corn seed oil, olive oil, castor oil and sesame oil, glycerol aliphatic ester, polyethylene glycol or sorbitan fatty acid ester May be used, but is not limited thereto. These may be used alone or in combination of two or more thereof.
- liquid carrier diluents such as water, ethanol or propylene glycol
- suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, micro Crystalline cellulose, aluminum metahydroxyde, bentonite, agar or tragacanth may be used, but is not limited thereto. These may be used alone or in combination of two or more thereof.
- the formulation of the present invention is a soap
- alkali metal salts of fatty acids fatty acid hemiester salts, fatty acid protein hydrolyzates, isethionates, lanolin derivatives, aliphatic alcohols, vegetable oils, glycerol, sugars and the like are used as carrier components. It may be, but is not limited thereto. These may be used alone or in combination of two or more thereof.
- the cosmetic composition of the present invention may be preferably a cosmetic composition for scalp hair care. Specifically, hair tonic, hair cream, hair lotion, hair shampoo, hair rinse, hair conditioner, hair spray, hair aerosol, pomade, powder, gel, hair pack, hair treatment, eyebrow regrowth, eyelash regrowth, eyelash nutrition But it is not limited thereto.
- the compound of Formula 1 or a cosmetically acceptable salt thereof is not limited in content, but may be included in an amount of 0.001 to 50% by weight, preferably 10% by weight, based on the total weight of the cosmetic composition.
- the present invention provides a food composition for preventing hair loss or promoting hair growth comprising acetoxychabicol acetate, a compound represented by the following Formula 1, or a food acceptable salt thereof as an active ingredient.
- the present invention also provides a food composition for preventing or improving hair loss comprising acetoxychabicol acetate, a compound represented by the formula (1), or a food acceptable salt thereof as an active ingredient.
- the compound of formula 1 of the present invention can be used as a food composition because it is derived from natural products and has been proven to be stable.
- the compound of Formula 1 or a food acceptable salt thereof is not limited in content, but may be included in an amount of about 0.001 to 50% by weight, preferably about 10% by weight, based on the total weight of the food composition.
- the composition may include additional ingredients that are commonly used in food compositions to improve the smell, taste, time and the like. For example, it may include vitamins A, C, D, E, B1, B2, B6, B12, niacin, biotin, folate, panthotenic acid, and the like.
- minerals such as zinc (Zn), iron (Fe), calcium (Ca), chromium (Cr), magnesium (Mg), manganese (Mn), copper (Cu). It may also contain amino acids such as lysine, tryptophan, cysteine, valine and the like.
- preservatives include potassium sorbate, sodium benzoate, salicylic acid, sodium dihydroacetate, etc.
- fungicides bleaching powder and highly bleaching powder, sodium hypochlorite, etc.
- antioxidants butylhydroxyanisol (BHA), butylhydroxytoluene (BHT)
- Colorants such as tar colors), colorants (such as sodium nitrite, sodium nitrite), bleach (sodium sulfite), seasonings (such as MSG glutamate), sweeteners (ducin, cyclate, saccharin, sodium, etc.),
- Food additives such as fragrances (vanillin, lactones, etc.), swelling agents (alum, potassium D-tartrate, etc.), reinforcing agents, emulsifiers, thickeners (pigments), coatings, gum herbicides, foam inhibitors, solvents, and improving agents. Can be added.
- the additive is selected according to the type of food and used in an appropriate amount.
- the term food acceptable salt means a salt in a form that can be used in food, even among salts in which cations and anions are bound by electrostatic attraction, and specific examples of the types thereof Includes examples of the “pharmaceutically acceptable salts” described above.
- the content of the compound represented by Formula 1 in the food composition of the present invention may be appropriately determined depending on the intended use.
- the compound represented by Formula 1 may be added at 0.0001 to 100% by weight based on the total weight of the food composition.
- the form of the food composition includes all foods in the usual sense.
- Foods to which the present invention can be applied include, for example, beverages, drinks, and health functional foods.
- the term "health functional food” means a food having an active health maintenance or promotion effect compared to a general food, and a health supplement food means a food for health supplement purposes.
- a health supplement food means a food for health supplement purposes.
- functional food, health food, health supplement food are used in.
- the food may be prepared in various forms such as tablets, capsules, powders, granules, liquids, pills, etc. in order to obtain useful effects.
- functional food is the same term as a food for special health use (FOSHU), in addition to nutrition, medical, medical effect processed to appear efficiently to regulate the bioregulatory function Means high food.
- FOSHU special health use
- the health functional food of the present invention by using the compound of Formula 1 or a food-acceptable salt thereof, it is possible to prepare a processed food with improved storage characteristics while modifying the characteristics of agricultural products, animal products or aquatic products.
- the dietary supplement is not particularly limited, but preferably margarine, fat continuous or water continuous or both continuous spreads, fat reduced spreads, chocolate, or chocolate coating or chocolate loaf. (fillings) or sweets such as bakery, ice cream, ice cream coatings, ice cream ingredients, dressings, mayonnaise, cheese, cream substitutes, dry soups, drinks, cereal bars, sauces, snack bars, dairy products, clinical nutrition foods, pediatric foods It may be used prepared in the form.
- Hair loss prevention or hair growth promoting composition comprising the compound of the formula (1) of the present invention as an active ingredient can be used for other animals, especially pets other than humans by appropriately modifying the formulation.
- composition of the present invention the method of preventing, ameliorating or treating hair loss using the composition of the present invention
- the present invention provides the use of the pharmaceutical composition described above for the preparation of a medicament for the prevention, treatment or amelioration of hair loss, or for the promotion of hair growth.
- the present invention also provides the use of the aforementioned pharmaceutical, quasi-drug, cosmetic or food composition for the prevention, treatment or amelioration of hair loss, or the promotion of hair growth.
- the present invention also provides a method for treating hair loss, comprising administering to a subject in need thereof a therapeutically effective amount of the above-mentioned pharmaceutical.
- the subject comprises a mammal, in particular a human.
- Acetoxychabicol acetate of the present invention has an excellent effect of promoting the growth of hair follicles to prevent hair loss and promote hair growth, and is derived from natural products and has no side effects, thus preventing hair loss or promoting hair growth. It can be used in various ways as a composition, quasi-drug composition, cosmetic composition, and food composition.
- FIG. 1 is a photograph observed through the animal experiments of the hair loss prevention and hair growth promoting effect of the acetoxychabicol acetate of the present invention.
- Figure 2 is a graph illustrating the hair follicle growth promoting effect of the acetoxychabicol acetate of the present invention in human hair follicle cell organ culture.
- Figure 4 is a photograph and graphs observed through animal experiments to prevent hair loss and hair growth promoting effect of the mass extract.
- Acetoxychabicol acetate used in this example was purchased from Abcam.
- mice Seven 7-week-old C57BL / 6 mice were divided into three experimental groups, in which all three groups received testosterone (10 ⁇ M solution, 100 ⁇ l foam) daily on mouse back skin, but the first group applied only testosterone and the second In group 3 and 3, acetoxychabicol acetate (10 ⁇ M solution, 50 ⁇ l foam) or minoxidil (2% solution, 50 ⁇ l foam) was applied to the back skin with testosterone from day 3, respectively. The experiment was conducted for 17 days based on the testosterone application date.
- acetoxychabicol acetate was confirmed to exhibit a similar degree of hair loss prevention and hair growth promoting effect compared to the effect of minoxidil (MNX) currently used as a hair loss treatment (FIG. 1). Therefore, acetoxychabicol acetate is expected to be used in various ways as a treatment for hair loss because it shows similar or more hair loss prevention and hair growth promoting effects with minoxidil, and there is no risk of side effects derived from natural products.
- Example 2 Hair follicle growth promoting effect of acetoxychabicol acetate
- Acetoxychabicol acetate used in this example was purchased from Abcam.
- Tissues were maintained in Williams E medium supplemented with 100 U penicillin / streptomycin, 10 ng / ml hydrocortisone, 10 ug / ml insulin and 2 mM L-glutamin under conditions of 5% CO2 and 37 ° C. 500 nM testosterone and each drug was treated in the medium for each concentration and 9 tissues were added and cultured for each condition. Change the medium every 3 days and measure the length of tissue growth after 6 days.
- the test group treated only with testosterone showed a hair follicle-producing hair of about 40% or more, while the test group treated with testosterone and acetoxychabicol acetate together had a similar degree to the control group without testosterone. It was confirmed that hair follicle generated hair length was maintained (FIG. 2). This demonstrates that hair follicle-producing hair growth inhibition by testosterone is restored by acetoxychabicol acetate.
- Extracts containing high concentrations of acetoxychabicol acetate were prepared using commercial bulk steels ( Alpinia galanga, Thailand) as follows.
- Example 4 Hair loss prevention and hair growth promoting effect of the mass extract
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Abstract
The present invention relates to a composition for preventing hair loss or promoting hair growth, comprising acetoxychavicol acetate as an active ingredient. More specifically, the present invention relates to a pharmaceutical composition, a quasi-drug composition, a cosmetic composition, and a health functional food for preventing hair loss or promoting hair growth, comprising acetoxychavicol acetate as an active ingredient. The acetoxychavicol acetate of the present invention has an excellent effect of accelerating the growth of hair follicles and thus, has an excellent effect of preventing hair loss and promoting hair growth; the acetoxychavicol acetate is also derived from natural products and thus has no side effects. Therefore, the acetoxychavicol acetate of the present invention can be variously utilized as a pharmaceutical composition, a quasi-drug composition, a cosmetic composition, and a health functional food for preventing hair loss or promoting hair growth.
Description
본 발명은 아세톡시차비콜 아세테이트(acetoxychavicol acetate)를 유효성분으로 포함하는 탈모 방지 또는 발모 촉진용 조성물에 관한 것이다.The present invention relates to a composition for preventing hair loss or promoting hair growth comprising acetoxychavicol acetate as an active ingredient.
구체적으로 본 발명은 아세톡시차비콜 아세테이트를 유효성분으로 포함하는 탈모 방지 또는 발모 촉진용 약학적 조성물, 의약외품 조성물, 화장료 조성물 및 식품 조성물에 관한 것이다.Specifically, the present invention relates to a pharmaceutical composition, a quasi-drug composition, a cosmetic composition, and a food composition for preventing hair loss or promoting hair growth comprising acetoxychabicol acetate as an active ingredient.
탈모는 정상적으로 모발이 존재해야 할 부위에 모발이 없는 상태를 말하며, 일반적으로 두피의 성모(굵은 모발)가 빠지는 것을 의미한다. 탈모는 노화에 의해 발생하는 것뿐만 아니라, 여러 가지 요인이 복합적으로 작용하여 젊은 연령대에서도 빈번하게 발생하는 질환이다. 탈모의 요인은 구체적으로 유전적 체질, 남성 호르몬의 작용 등과 같은 내적인 요인, 일상생활에서의 스트레스, 식생활 습관, 두피에서의 과산화지질의 축적 등과 같은 외적인 요인을 들 수 있다. 최근에는 남성형 탈모뿐만 아니라 여성들의 비만성 탈모를 비롯하여 젊은 층에서의 탈모가 점차 확산되어가는 추세에 있으며, 이러한 탈모 현상을 개선하기 위해 많은 종류의 탈모 치료제, 육모제 등이 시판되고 있다.Hair loss refers to a condition in which there is no hair in the area where hair should normally exist, and generally means that the hair of the scalp (coarse hair) falls out. Hair loss is a disease that occurs not only by aging but also by many factors in combination with young age. Specifically, the cause of hair loss may include internal factors such as genetic constitution and the action of testosterone, external stress such as daily stress, dietary habits, and accumulation of lipid peroxide in the scalp. In recent years, hair loss in young people, including obesity hair loss in women as well as male hair loss has been gradually spread, and many kinds of hair loss treatment agents, hair growth agents, etc. are commercially available to improve the hair loss phenomenon.
시판되고 있는 대표적인 탈모 치료제인 미녹시딜(Minoxidil)은 본래 혈압 강하를 위해 개발된 고혈압 치료제였으나, 사용상 부작용으로 발모현상이 나타나면서 현재에는 발모제로 더욱 유명해진 약물이다. 그러나 미녹시딜 제제는 과다 사용 시 두피소양증, 홍반, 각질 등의 접촉 피부염이나 다모증 등의 부작용이 발생할 수 있는 것으로 알려져 있다(J Korean Med Assoc 2013 January; 56(1): 45-54).Minoxidil (minoxidil), a typical anti-hair loss treatment on the market, was originally developed for the treatment of hypertension, but it is a drug that has become more famous as a hair regrowth agent due to side effects of use. However, minoxidil preparations are known to cause side effects such as contact dermatitis or hirsutism, such as scalp pruritus, erythema, and keratin overuse (J Korean Med Assoc 2013 January; 56 (1): 45-54).
또 다른 대표적인 탈모 치료제제인 프로페시아(Propesia)는 남성형 탈모증의 발병에 중요한 역할을 하는 5-알파-환원효소 2형 효소를 차단시켜 테스토스테론이 디하이드로테스토스테론(Dihydrotestosterone; DHT)으로 변화되는 것을 억제하여 탈모를 호전시키거나 탈모의 진행을 억제시키는 것으로 알려져 있다. 프로페시아는 탈모 방지 효과가 우수한 것으로 알려져 있으나, 이를 제조하는데 있어 사용되는 시약이 고가이며 독성이 있는 문제가 있으며, 스테로이드 호르몬의 생성 자체를 인위적으로 차단하는 방식으로 작용하는 것이기 때문에 여러 부작용이 발생할 수 있는 위험이 있다. 이에, 탈모 방지 및 발모 촉진 효능이 우수하면서도 부작용이 없는 안전한 치료제의 개발이 여전히 요구되고 있는 실정이다.Another representative hair loss treatment agent, Propesia, blocks the 5-alpha-reductase type 2 enzyme, which plays an important role in the development of androgenetic alopecia, thereby inhibiting the change of testosterone to dihydrotestosterone (DHT). It is known to improve or inhibit the progression of hair loss. Propecia is known to have excellent hair loss prevention effects, but the reagents used to manufacture it are expensive and toxic, and because it acts in a way that artificially blocks the production of steroid hormones itself, many side effects may occur. There is a danger. Therefore, there is still a need for the development of a safe treatment agent having excellent efficacy of preventing hair loss and promoting hair growth, but having no side effects.
본 발명은 아세톡시차비콜 아세테이트(acetoxychavicol acetate)를 유효성분으로 포함하는 탈모 방지 또는 발모 촉진용 조성물을 제공하는 것을 목적으로 한다.An object of the present invention is to provide a composition for preventing hair loss or promoting hair growth comprising acetoxychavicol acetate (acetoxychavicol acetate) as an active ingredient.
구체적으로 본 발명은 아세톡시차비콜 아세테이트를 유효성분으로 포함하는 탈모 방지 또는 발모 촉진용 약학적 조성물, 의약외품 조성물, 화장료 조성물 및 식품 조성물을 제공하는 것을 목적으로 한다.Specifically, an object of the present invention is to provide a pharmaceutical composition for preventing hair loss or promoting hair growth, quasi-drug composition, cosmetic composition and food composition comprising acetoxychabicol acetate as an active ingredient.
약학적 조성물Pharmaceutical composition
본 발명은 하기 화학식 1로 표시되는 화합물인 아세톡시차비콜 아세테이트(acetoxychavicol acetate) 또는 이의 약학적으로 허용되는 염을 유효성분으로 포함하는 탈모 방지 또는 발모 촉진용 약학적 조성물을 제공한다.The present invention provides a pharmaceutical composition for preventing hair loss or promoting hair growth comprising acetoxychavicol acetate (acetoxychavicol acetate) or a pharmaceutically acceptable salt thereof as an active ingredient.
[화학식 1][Formula 1]
본 발명에서 상기 화학식1의 화합물은 화학적으로 합성하거나 천연 물질로부터 분리할 수 있으며, 국내외에서 시판되는 것을 구입하여 사용할 수도 있다. 본 발명에서 상기 화학식1의 화합물을 식물로부터 분리하는 경우, 식물의 종류는 특별히 제한되지 아니하나 바람직하게는 대량강(Alpinia galanga)의 근경을 이용하여 분리할 수 있다. 또한 아세톡시차비콜 아세테이트를 고농도로 함유하는 식물추출물을 제조할 수도 있다.In the present invention, the compound of Formula 1 may be chemically synthesized or separated from natural materials, and may be purchased and used commercially at home and abroad. In the present invention, when the compound of Formula 1 is separated from a plant, the type of plant is not particularly limited, but may be separated using a root diameter of Alpinia galanga . It is also possible to prepare plant extracts containing a high concentration of acetoxychabicol acetate.
본 발명자들은 대량강(Alpinia galanga, 태국산)의 근경을 이용하여 아세톡시차비콜 아세테이트 고함유 추출물을 제조할 수 있다. 구체적으로 본 발명의 실시예에 의하면, 대량강 근경 생체 50 g을 세절 한 후, 70% 수용성 에탄올을 250 ml 넣고 2시간 동안 초음파 추출을 2회 반복하였다. 상기 방법에 의해 얻어진 추출물을 여과한 후, 여액을 40℃~50℃에서 감압농축한 다음, 동결건조하여 대량강 근경의 70% 에탄올 추출물 2.2g(수율 4.4%)을 수득하였다. 상기 수득된 추출물 중의 아세톡시차비콜 아세테이트 함유량은 14.61%인 것으로 확인되었다(도 3).The present inventors can prepare a high extract of acetoxychabicol acetate using the root of the mass steel ( Alpinia galanga, Thailand). In detail, according to the embodiment of the present invention, after cutting 50 g of the bulk rhizome living body, 250 ml of 70% aqueous ethanol was added and the ultrasonic extraction was repeated twice for 2 hours. After filtering the extract obtained by the above method, the filtrate was concentrated under reduced pressure at 40 ℃ ~ 50 ℃, and then lyophilized to give 2.2 g (yield 4.4%) of 70% ethanol extract of the mass root diameter. The acetoxychabicol acetate content in the obtained extract was found to be 14.61% (FIG. 3).
본 발명의 실시예에서 아세톡시차비콜 아세테이트 단일 화합물을 이용한 실험의 경우에는 Abcam사로부터 구입하여 사용하였다.In the case of the experiment using the acetoxychabicol acetate single compound in the embodiment of the present invention was purchased from Abcam.
본 발명의 화학식 1의 화합물은 모낭의 성장을 촉진하는 효능을 갖는다.The compound of formula 1 of the present invention has the effect of promoting the growth of hair follicles.
구체적으로 본 발명의 실시예에서, 사람 모낭세포(n=36)를 4개의 그룹으로 나누어, 제1군은 약물을 처리하지 않은 대조군(control), 제2군은 테스토스테론 500 nM 처리, 제3군은 테스토스테론 500 nM과 아세톡시차비콜 아세테이트 100 nM 처리, 제4군은 테스토스테론 500 nM과 아세톡시차비콜 아세테이트 200 nM을 처리하여 기관 배양을 수행한 결과, 테스토스테론만 처리한 실험군에서는 모낭의 크기가 약 40% 이상의 감소를 보인 반면, 테스토스테론과 아세톡시차비콜 아세테이트를 함께 처리한 실험군에서는 모두 테스토스테론을 처리하지 않은 대조군과 유사한 정도로 모낭의 크기가 유지되는 것을 확인하였다(도 2). 이는 테스토스테론에 의한 모낭 크기 감소 및 그에 따른 발모 억제가 아세톡시차비콜 아세테이트에 의해 회복됨을 입증하는 것이다.Specifically, in the embodiment of the present invention, human hair follicle cells (n = 36) divided into four groups, the first group is a control (control) not treated with the drug, the second group is treated with testosterone 500 nM, the third group In the test group treated with 500 nM of silver testosterone and 100 nM of acetoxycarbicol acetate and 200 nM of testosterone and 200 nM of acetoxycarbicol acetate, hair follicles in the test group treated only with testosterone had a small size. While showing a reduction of more than 40%, both experimental groups treated with testosterone and acetoxychabicol acetate were confirmed to maintain the size of the hair follicles to a similar degree as the control group not treated with testosterone (FIG. 2). This demonstrates that the reduction in hair follicle size and thus hair growth inhibition by testosterone is restored by acetoxychabicol acetate.
본 발명의 화학식 1의 화합물은 피부 세포에서 활성산소(ROS)의 생성을 억제하는 효능을 갖는다.The compound of formula 1 of the present invention has the effect of inhibiting the production of free radicals (ROS) in skin cells.
본 발명의 화학식 1의 화합물은 피부 세포에서 NADPH 산화효소(Nox)의 활성을 억제하는 효능을 갖는다.The compound of formula 1 of the present invention has the effect of inhibiting the activity of NADPH oxidase (Nox) in skin cells.
본 발명은 또한, 하기 화학식 1로 표시되는 화합물인 아세톡시차비콜 아세테이트(acetoxychavicol acetate) 또는 이의 약학적으로 허용되는 염을 유효성분으로 포함하는 탈모의 예방 또는 치료용 약학적 조성물을 제공한다.The present invention also provides a pharmaceutical composition for the prevention or treatment of hair loss comprising acetoxychavicol acetate (acetoxychavicol acetate) or a pharmaceutically acceptable salt thereof as an active ingredient as a compound represented by the following formula (1).
[화학식 1][Formula 1]
본 발명에서 사용되는 용어, 약학적으로 허용되는 염이란, 양이온과 음이온이 정전기적 인력에 의해 결합하고 있는 물질인 염 중에서도 약제학적으로 사용될 수 있는 형태의 염을 의미하는데, 통상적으로 금속염, 유기 염기와의 염, 무기산과의 염, 유기산과의 염, 염기성 또는 산성 아미노산과의 염 등이 될 수 있다. 예를 들어, 금속염으로는 알칼리 금속염(나트륨염, 칼륨염 등), 알칼리 토금속염(칼슘염, 마그네슘염, 바륨염 등), 알루미늄염 등이 될 수 있고; 유기 염기와의 염으로는 트리에틸아민, 피리딘, 피콜린, 2,6-루티딘, 에탄올아민, 디에탄올아민, 트리에탄올아민, 시클로헥실아민, 디시클로헥실아민, N,N-디벤질에틸렌디아민 등과의 염이 될 수 있으며; 무기산과의 염으로는 염산, 브롬화수소산, 질산, 황산, 인산 등과의 염이 될 수 있고; 유기산과의 염으로는 포름산, 아세트산, 트리플루오로아세트산, 프탈산, 푸마르산, 옥살산, 타르타르산, 말레인산, 시트르산, 숙신산, 메탄술폰산, 벤젠술폰산, p-톨루엔술폰산 등과의 염이 될 수 있으며; 염기성 아미노산과의 염으로는 아르기닌, 라이신, 오르니틴 등과의 염이 될 수 있고; 산성 아미노산과의 염으로는 아스파르트산, 글루탐산 등과의 염이 될 수 있다.As used herein, the term pharmaceutically acceptable salt means a salt in a form that can be used pharmaceutically among salts in which cations and anions are bound by electrostatic attraction, and are generally metal salts and organic bases. Salts with, inorganic acids, salts with organic acids, salts with basic or acidic amino acids, and the like. For example, the metal salt may be an alkali metal salt (sodium salt, potassium salt, etc.), alkaline earth metal salt (calcium salt, magnesium salt, barium salt, etc.), aluminum salt, or the like; Salts with organic bases include triethylamine, pyridine, picoline, 2,6-lutidine, ethanolamine, diethanolamine, triethanolamine, cyclohexylamine, dicyclohexylamine, N, N-dibenzylethylenediamine Salts and the like; Salts with inorganic acids can be salts with hydrochloric acid, hydrobromic acid, nitric acid, sulfuric acid, phosphoric acid, and the like; Salts with organic acids can be salts with formic acid, acetic acid, trifluoroacetic acid, phthalic acid, fumaric acid, oxalic acid, tartaric acid, maleic acid, citric acid, succinic acid, methanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, and the like; Salts with basic amino acids can be salts with arginine, lysine, ornithine and the like; Salts with acidic amino acids can be salts with aspartic acid, glutamic acid and the like.
본 발명의 약학적 조성물은 화학식 1의 화합물 또는 이의 약학적으로 허용되는 염을 유효 성분으로 포함하는 것 이외에 약학적으로 허용 가능한 담체를 추가로 포함할 수 있다.The pharmaceutical composition of the present invention may further include a pharmaceutically acceptable carrier in addition to including the compound of formula 1 or a pharmaceutically acceptable salt thereof as an active ingredient.
본 발명에서 상기 담체의 종류는 특별히 제한되지 아니하며 당해 기술 분야에서 통상적으로 사용되는 담체라면 어느 것이든 사용할 수 있다. 상기 담체의 비제한적인 예로는, 식염수, 멸균수, 링거액, 완충 식염수, 알부민 주사 용액, 락토오스, 덱스트로오스, 수크로오스, 솔비톨, 만니톨, 자일리톨, 에리스리톨, 말티톨, 말토 덱스트린, 글리세롤, 에탄올 등을 들 수 있다. 이들은 단독으로 사용되거나 2 종 이상을 혼합하여 사용될 수 있다.In the present invention, the type of the carrier is not particularly limited, and any carrier may be used as long as it is commonly used in the art. Non-limiting examples of the carrier include saline, sterile water, Ringer's solution, buffered saline, albumin injection solution, lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, maltodextrin, glycerol, ethanol, and the like. Can be. These may be used alone or in combination of two or more thereof.
또한, 본 발명의 약학적 조성물은 필요한 경우, 부형제, 희석제, 항산화제, 완충액 또는 정균제 등 기타 약학적으로 허용 가능한 첨가제들을 첨가하여 사용할 수 있으며, 충진제, 증량제, 습윤제, 붕해제, 분산제, 계면 활성제, 결합제 또는 윤활제 등을 부가적으로 첨가하여 사용할 수 있다.In addition, the pharmaceutical composition of the present invention may be used, if necessary, by adding other pharmaceutically acceptable additives such as excipients, diluents, antioxidants, buffers or bacteriostatic agents, fillers, extenders, wetting agents, disintegrants, dispersants, surfactants , Binders or lubricants may be additionally added and used.
본 발명의 약학적 조성물에 있어서, 화학식 1의 화합물 또는 이의 약학적으로 허용되는 염은 상기 약학적 조성물의 전체의 중량을 기준으로 0.00001 중량% 내지 99.99 중량%로 포함될 수 있으며, 바람직하게는 1 중량% 내지 99.99 중량%, 보다 바람직하게는 10 중량% 내지 99.99 중량%, 더욱 바람직하게는 50 중량% 내지 99.99 중량%로 포함될 수 있으며, 약학적 조성물의 전체 함량으로도 포함될 수 있다.In the pharmaceutical composition of the present invention, the compound of Formula 1 or a pharmaceutically acceptable salt thereof may be included in an amount of 0.00001% to 99.99% by weight based on the total weight of the pharmaceutical composition, preferably 1% by weight. % To 99.99% by weight, more preferably 10% to 99.99% by weight, more preferably 50% to 99.99% by weight, and may also be included in the total content of the pharmaceutical composition.
본 발명의 약학적 조성물은 경구 투여 또는 비경구 투여를 위한 적합한 다양한 제형으로 제제화되어 사용될 수 있다.The pharmaceutical compositions of the present invention can be formulated and used in a variety of formulations suitable for oral or parenteral administration.
상기 경구 투여용 제제의 비제한적인 예로는, 트로키제(troches), 로젠지(lozenge), 정제, 수용성 현탁액, 유성 현탁액, 조제 분말, 과립, 에멀젼, 하드 캡슐, 소프트 캡슐, 시럽 또는 엘릭시르제 등을 들 수 있다.Non-limiting examples of the formulation for oral administration include troches, lozenges, tablets, aqueous suspensions, oily suspensions, prepared powders, granules, emulsions, hard capsules, soft capsules, syrups or elixirs, and the like. Can be mentioned.
본 발명의 약학적 조성물을 경구 투여용으로 제제화하기 위하여, 락토오스, 사카로오스, 솔비톨, 만니톨, 전분, 아밀로펙틴, 셀룰로오스 또는 젤라틴 등과 같은 결합제; 디칼슘 포스페이트 등과 같은 부형제; 옥수수 전분 또는 고구마 전분 등과 같은 붕해제; 스테아르산 마그네슘, 스테아르산 칼슘, 스테아릴 푸마르산 나트륨 또는 폴리에틸렌 글리콜 왁스 등과 같은 윤활유 등을 사용할 수 있으며, 감미제, 방향제, 시럽제 등도 사용할 수 있다. 나아가 캡슐제의 경우에는 상기 언급한 물질 외에도 지방유와 같은 액체 담체 등을 추가로 사용할 수 있다.In order to formulate the pharmaceutical composition of the present invention for oral administration, a binder such as lactose, saccharose, sorbitol, mannitol, starch, amylopectin, cellulose or gelatin and the like; Excipients such as dicalcium phosphate and the like; Disintegrants such as corn starch or sweet potato starch; Lubricants such as magnesium stearate, calcium stearate, sodium stearyl fumarate or polyethylene glycol wax and the like can be used, and sweeteners, fragrances, syrups and the like can also be used. Furthermore, in the case of a capsule, a liquid carrier such as fatty oil may be additionally used in addition to the above-mentioned materials.
상기 비경구용 제제의 비제한적인 예로는, 주사액, 좌제, 호흡기 흡입용 분말, 스프레이용 에어로졸제, 연고, 도포용 파우더, 오일, 크림 등을 들 수 있다.Non-limiting examples of the parenteral preparations include injection liquids, suppositories, respiratory inhalation powders, spray aerosols, ointments, application powders, oils, creams, and the like.
본 발명의 상기 약학적 조성물을 비경구 투여용으로 제제화하기 위하여, 멸균된 수용액, 비수성용제, 현탁제, 유제, 동결 건조 제제, 외용제 등을 사용할 수 있으며, 상기 비수성용제, 현탁제로는 프로필렌글리콜, 폴리에틸렌글리콜, 올리브 오일과 같은 식물성 기름, 에틸올레이트와 같은 주사 가능한 에스테르 등이 사용될 수 있다.In order to formulate the pharmaceutical composition for parenteral administration, a sterile aqueous solution, a non-aqueous solvent, a suspension, an emulsion, a freeze-dried preparation, an external preparation, and the like may be used. The non-aqueous solvent and the suspension may be propylene glycol, Polyethyleneglycol, vegetable oils such as olive oil, injectable esters such as ethyloleate and the like can be used.
본 발명의 약학적 조성물을 주사액으로 제제화하는 경우, 본 발명의 상기 조성물을 안정제 또는 완충제와 함께 물에서 혼합하여 용액 또는 현탁액으로 제조하고 이를 앰플(ampoule) 또는 바이알(vial)의 단위 투여용으로 제제화할 수 있다.When formulating the pharmaceutical composition of the present invention into an injection solution, the composition of the present invention is mixed in water with a stabilizer or buffer to prepare a solution or suspension which is formulated for unit administration of ampoules or vials. can do.
본 발명의 약학적 조성물을 에어로졸제로 제제화하는 경우, 수분산된 농축물 또는 습윤 분말이 분산되도록 추진제 등이 첨가제와 함께 배합할 수 있다.When formulating the pharmaceutical composition of the present invention with an aerosol, a propellant or the like may be combined with the additive to disperse the dispersed dispersion or the wet powder.
본 발명의 약학적 조성물을 연고, 크림, 도포용 파우더, 오일, 피부 외용제 등으로 제제화하는 경우에는, 동물성 유, 식물성 유, 왁스, 파라핀, 전분, 트라칸트, 셀룰로오스 유도체, 폴리에틸렌 글리콜, 실리콘, 벤토나이트, 실리카, 탈크, 산화 아연 등을 담체로 사용하여 제제화할 수 있다.When the pharmaceutical composition of the present invention is formulated into an ointment, a cream, a powder for application, an oil, an external skin preparation, etc., animal oil, vegetable oil, wax, paraffin, starch, tracant, cellulose derivative, polyethylene glycol, silicone, bentonite , Silica, talc, zinc oxide and the like can be formulated using a carrier.
본 발명의 약학적 조성물의 약학적 유효량, 유효 투여량은 상기 약학적 조성물의 제제화 방법, 투여 방식, 투여 시간 및/또는 투여 경로 등에 의해 다양해질 수 있으며, 상기 약학 조성물의 투여로 달성하고자 하는 반응의 종류와 정도, 투여 대상이 되는 개체의 종류, 연령, 체중, 일반적인 건강 상태, 질병의 증세나 정도, 성별, 식이, 배설, 해당 개체에 동시 또는 이시에 함께 사용되는 약물 기타 조성물의 성분 등을 비롯한 여러 인자 및 의약 분야에서 잘 알려진 유사 인자에 따라 다양해질 수 있으며, 당해 기술 분야에서 통상의 지식을 가진 자는 목적하는 치료에 효과적인 투여량을 용이하게 결정하고 처방할 수 있다.Pharmaceutically effective amounts, effective dosages of the pharmaceutical compositions of the present invention may vary depending on the formulation method, mode of administration, time of administration and / or route of administration of the pharmaceutical composition, and the reaction to be achieved by the administration of the pharmaceutical composition. The type and extent of the subject, type, age, weight, general state of health, condition and extent of the disease, sex, diet, excretion, and components of the drug or other composition used concurrently or simultaneously with the subject. And various similar factors well known in the medical arts, and those skilled in the art can readily determine and prescribe a dosage effective for the desired treatment.
본 발명의 약학적 조성물의 투여는 하루에 1회 투여될 수 있고, 수회에 나누어 투여될 수도 있다. 본 발명의 약학적 조성물은 개별 치료제로 투여하거나 다른 치료제와 병용하여 투여될 수 있고 종래의 치료제와는 순차적 또는 동시에 투여될 수 있다. 상기 요소를 모두 고려하여 부작용 없이 최소한의 양으로 최대 효과를 얻을 수 있는 양으로 투여할 수 있으며, 이는 당업자에 의해 용이하게 결정될 수 있다.Administration of the pharmaceutical composition of the present invention may be administered once a day, may be divided into several times. The pharmaceutical compositions of the present invention may be administered as individual therapeutic agents or in combination with other therapeutic agents and may be administered sequentially or simultaneously with conventional therapeutic agents. All of the above factors can be considered and administered in an amount that can obtain the maximum effect in a minimum amount without side effects, which can be easily determined by those skilled in the art.
본 발명의 약학적 조성물의 투여 경로 및 투여 방식은 각각 독립적일 수 있으며, 목적하는 해당 부위에 상기 약학적 조성물이 도달할 수 있는 한, 특별한 제한 없이 임의의 투여 경로 및 투여 방식에 따를 수 있다. 상기 약학적 조성물은 경구 투여 또는 비경구 투여 방식으로 투여할 수 있다.The route of administration and mode of administration of the pharmaceutical compositions of the present invention may be independent of each other, and may be any route of administration and mode of administration without particular limitation, so long as the pharmaceutical composition can reach the desired site of interest. The pharmaceutical composition may be administered by oral or parenteral administration.
상기 비경구 투여 방법으로는, 정맥 내 투여, 복강 내 투여, 근육 내 투여, 경피 투여 또는 피하 투여 등을 이용할 수 있으며, 상기 조성물을 질환 부위에 도포하거나 분무, 흡입하는 방법 또한 이용할 수 있으나 이에 제한되지 않는다.As the parenteral administration method, intravenous administration, intraperitoneal administration, intramuscular administration, transdermal administration or subcutaneous administration may be used, and the method of applying, spraying or inhaling the composition to a diseased site may also be used, but the present invention is not limited thereto. It doesn't work.
본 발명의 약학적 조성물은 바람직하게는 모발, 피부 또는 두피에 직접 도포 또는 산포하는 방법으로 사용될 수 있다.The pharmaceutical composition of the present invention may be preferably used in a method of directly applying or spreading on hair, skin or scalp.
본 발명에서 사용되는 용어, “모발”은 머리의 모근 및 모낭, 머리카락, 속눈썹, 겉눈썹, 수염 등 신체 전반에 모근 및 모낭이 있는 모든 부위를 포함할 수 있다.As used herein, the term “hair” may include all parts of the hair root and hair follicles throughout the body, such as hair roots and hair follicles of hair, hair, eyelashes, eyelashes, and beards.
의약외품 조성물Quasi-drug composition
본 발명은 하기 화학식 1로 표시되는 화합물인 아세톡시차비콜 아세테이트 또는 이의 약학적으로 허용되는 염을 유효성분으로 포함하는 탈모 방지 또는 발모 촉진용 의약외품 조성물을 제공한다.The present invention provides a quasi-drug composition for preventing hair loss or promoting hair growth comprising acetoxychabicol acetate, or a pharmaceutically acceptable salt thereof, as a compound represented by the following Formula 1.
[화학식 1][Formula 1]
본 발명에서 사용되는 용어, “의약외품”은 사람이나 동물의 질병을 진단, 치료, 개선, 경감, 처치 또는 예방할 목적으로 사용되는 물품들 중 의약품보다 작용이 경미한 물품들을 의미하는 것으로, 예를 들어 약사법에 따르면 의약외품이란 의약품의 용도로 사용되는 물품을 제외한 것으로, 사람ㆍ동물의 질병 치료나 예방에 쓰이는 제품, 인체에 대한 작용이 경미하거나 직접 작용하지 않는 제품 등이 포함된다.As used herein, the term “quasi drug” refers to articles that have a lesser action than pharmaceuticals among articles used for the purpose of diagnosing, treating, ameliorating, alleviating, treating, or preventing a disease in humans or animals. According to the article, quasi-drugs exclude products used for the purpose of medicines, and include products used for the treatment or prevention of diseases of humans and animals, and products with slight or no direct action on the human body.
본 발명의 상기 화학식 1의 화합물을 의약외품 첨가물로 사용하는 경우, 이를 그대로 첨가하거나 다른 의약외품 또는 의약외품 성분과 함께 사용될 수 있고, 통상적인 방법에 따라 적절하게 사용될 수 있다. 함께 사용되는 다른 성분들과의 혼합비율은 사용 목적(예를 들어, 예방, 개선 또는 치료적 처치)에 따라 적합하게 결정될 수 있다.When the compound of Formula 1 of the present invention is used as an quasi-drug additive, it may be added as it is or used with other quasi-drug or quasi-drug components, and may be appropriately used according to a conventional method. The mixing ratio with other ingredients used together may be suitably determined depending on the purpose of use (eg, prevention, improvement or therapeutic treatment).
상기 의약외품 조성물의 예로는 샴푸, 린스 등의 두피 모발 케어 조성물, 바디 클렌저, 폼, 비누, 마스크, 연고제, 크림, 로션, 에센스, 스프레이 등을 들 수 있으나, 이에 제한되는 것은 아니다.Examples of the quasi-drug composition may include, but are not limited to, scalp hair care compositions such as shampoos and rinses, body cleansers, foams, soaps, masks, ointments, creams, lotions, essences, sprays, and the like.
본 발명의 화학식 1의 화합물 또는 이의 약학학적으로 허용되는 염을 유효성분으로 포함하는 의약외품 조성물은 바람직하게는 두피 모발 케어용 조성물일 수 있다.The quasi-drug composition comprising the compound of formula 1 of the present invention or a pharmaceutically acceptable salt thereof as an active ingredient may preferably be a composition for scalp hair care.
본 발명에서 사용되는 용어, “두피 모발 케어용 조성물”은 두피 및 모발의 손상을 방지 또는 완화해주는 조성물을 의미한다. 두피 모발 케어용 조성물의 제형은 샴푸, 린스, 에센스, 영양제, 세럼, 마사지 크림, 로션, 팩제 등 일 수 있으나 이에 제한되지 않는다.As used herein, the term “composition for scalp hair care” refers to a composition that prevents or alleviates damage to the scalp and hair. The formulation of the scalp hair care composition may be, but is not limited to, shampoo, rinse, essence, nutrient, serum, massage cream, lotion, pack, and the like.
상기 화학식 1의 화합물 또는 이의 약학적으로 허용되는 염은 그 함량이 제한되는 것은 아니나, 의약외품 조성물의 총 중량에 대하여 0.001 내지 50 중량%, 바람직하게는 10 중량% 내외로 포함될 수 있다.The compound of Formula 1 or a pharmaceutically acceptable salt thereof may be included in an amount of about 0.001 to 50% by weight, preferably about 10% by weight, based on the total weight of the quasi-drug composition.
화장료 조성물Cosmetic composition
본 발명은 하기 화학식 1로 표시되는 화합물인 아세톡시차비콜 아세테이트 또는 이의 화장품학적으로 허용되는 염을 유효성분으로 포함하는 탈모 방지 또는 발모 촉진용 화장료 조성물을 제공한다.The present invention provides a cosmetic composition for preventing hair loss or promoting hair growth comprising acetoxychabicol acetate or a cosmetically acceptable salt thereof as an active ingredient, which is a compound represented by Formula 1 below.
[화학식 1][Formula 1]
본 발명에서 사용되는 용어, “화장품학적으로 허용되는 염”은, 양이온과 음이온이 정전기적 인력에 의해 결합하고 있는 물질인 염 중에서도 화장품학적으로 사용될 수 있는 형태의 염을 의미하며, 그 종류에 대한 구체적인 예는 상술한 “약학적으로 허용되는 염”의 예를 포함한다.As used herein, the term “cosmetically acceptable salts” refers to salts that can be used cosmetically even among salts in which cations and anions are bonded by electrostatic attraction. Specific examples include examples of the "pharmaceutically acceptable salts" described above.
본 발명의 상기 화장료 조성물의 제형은 예를 들어, 용액, 샴푸, 린스, 외용 연고, 크림, 폼, 영양 화장수, 유연 화장수, 팩, 유연수, 유액, 메이크업 베이스, 에센스, 액체 세정료, 입욕제, 선 스크린 크림, 선 오일, 현탁액, 유탁액, 페이스트, 겔, 로션, 파우더, 비누, 계면 활성제-함유 클렌징, 오일, 분말 파운데이션, 유탁액 파운데이션, 왁스 파운데이션, 패취, 스프레이 등을 들 수 있으나 이에 제한되지 않는다.Formulation of the cosmetic composition of the present invention is, for example, solution, shampoo, rinse, external ointment, cream, foam, nourishing lotion, flexible lotion, pack, flexible water, latex, makeup base, essence, liquid cleanser, bath, sun Screen creams, sun oils, suspensions, emulsions, pastes, gels, lotions, powders, soaps, surfactant-containing cleansing, oils, powder foundations, emulsion foundations, wax foundations, patches, sprays, and the like. Do not.
본 발명의 상기 화장료 조성물은 일반 화장료에 배합되는 화장품학적으로 허용 가능한 담체를 1 종 이상 추가로 포함할 수 있으며, 통상의 성분으로 예를 들면 유분, 물, 계면 활성제, 보습제, 저급 알코올, 증점제, 킬레이트제, 색소, 방부제, 향료 등을 적절히 배합할 수 있으나, 이에 제한되는 것은 아니다.The cosmetic composition of the present invention may further include one or more cosmetically acceptable carriers formulated in general cosmetics, and as common components, for example, oil, water, surfactants, moisturizers, lower alcohols, thickeners, Chelating agents, pigments, preservatives, fragrances and the like can be appropriately blended, but is not limited thereto.
본 발명의 화장료 조성물에 포함되는 화장품학적으로 허용 가능한 담체는 화장료 조성물의 제형에 따라 다양할 수 있다.The cosmetically acceptable carrier included in the cosmetic composition of the present invention may vary depending on the formulation of the cosmetic composition.
본 발명의 제형이 연고, 페이스트, 크림 또는 젤인 경우에는, 담체 성분으로서 동물성 유, 식물성 유, 왁스, 파라핀, 전분, 트라가칸트, 셀룰로오스 유도체, 폴리에틸렌 글리콜, 실리콘, 벤토나이트, 실리카, 탈크, 산화 아연 등이 이용될 수 있으나, 이에 제한되는 것은 아니다. 이들은 단독으로 사용되거나 2 종 이상 혼합되어 사용될 수 있다.When the formulation of the present invention is an ointment, paste, cream or gel, the carrier component is animal oil, vegetable oil, wax, paraffin, starch, tragacanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc, zinc oxide Etc. may be used, but is not limited thereto. These may be used alone or in combination of two or more thereof.
본 발명의 제형이 파우더 또는 스프레이인 경우에는, 담체 성분으로서 락토스, 탈크, 실리카, 알루미늄 히드록사이드, 칼슘 실리케이트, 폴리아미드 파우더 등이 이용될 수 있고, 특히 스프레이인 경우에는 추가적으로 클로로플루오로히드로카본, 프로판/부탄 또는 디메틸 에테르와 같은 추진제를 포함할 수 있으나, 이에 제한되는 것은 아니다. 이들은 단독으로 사용되거나 2 종 이상 혼합되어 사용될 수 있다.When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate, polyamide powder, and the like can be used, in particular, in the case of a spray, additionally chlorofluorohydrocarbons. Propellant, such as, but not limited to, propane / butane or dimethyl ether. These may be used alone or in combination of two or more thereof.
본 발명의 제형이 용액 또는 유탁액인 경우에는, 담체 성분으로서 용매, 용해화제 또는 유탁화제 등이 이용될 수 있으며, 예컨대 물, 에탄올, 이소프로판올, 에틸 카보네이트, 에틸 아세테이트, 벤질 알코올, 벤질 벤조에이트, 프로필렌 글리콜, 1,3-부틸글리콜 오일 등이 이용될 수 있고, 특히, 목화씨 오일, 땅콩 오일, 옥수수 배종 오일, 올리브 오일, 피마자 오일 및 참깨 오일, 글리세롤 지방족 에스테르, 폴리에틸렌 글리콜 또는 소르비탄의 지방산 에스테르가 이용될 수 있으나, 이에 제한되는 것은 아니다. 이들은 단독으로 사용되거나 2 종 이상 혼합되어 사용될 수 있다.When the formulation of the present invention is a solution or emulsion, a solvent, solubilizer or emulsion may be used as the carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, Propylene glycol, 1,3-butylglycol oil, and the like can be used, and in particular, cottonseed oil, peanut oil, corn seed oil, olive oil, castor oil and sesame oil, glycerol aliphatic ester, polyethylene glycol or sorbitan fatty acid ester May be used, but is not limited thereto. These may be used alone or in combination of two or more thereof.
본 발명의 제형이 현탁액인 경우에는, 담체 성분으로서 물, 에탄올 또는 프로필렌글리콜과 같은 액상의 희석제, 에톡실화 이소스테아릴 알코올, 폴리옥시에틸렌 소르비톨 에스테르 및 폴리옥시에틸렌 소르비탄 에스테르와 같은 현탁제, 미소결정성 셀룰로오스, 알루미늄 메타하이드록시드, 벤토나이트, 아가 또는 트라가칸트 등이 이용될 수 있으나, 이에 제한되는 것은 아니다. 이들은 단독으로 사용되거나 2 종 이상 혼합되어 사용될 수 있다.When the dosage form of the present invention is a suspension, liquid carrier diluents such as water, ethanol or propylene glycol, suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, micro Crystalline cellulose, aluminum metahydroxyde, bentonite, agar or tragacanth may be used, but is not limited thereto. These may be used alone or in combination of two or more thereof.
본 발명의 제형이 비누인 경우에는, 담체 성분으로서 지방산의 알칼리 금속 염, 지방산 헤미에스테르 염, 지방산 단백질 히드롤리제이트, 이세티오네이트, 라놀린 유도체, 지방족 알코올, 식물성 유, 글리세롤, 당 등이 이용될 수 있으나, 이에 제한되는 것은 아니다. 이들은 단독으로 사용되거나 2 종 이상 혼합되어 사용될 수 있다.When the formulation of the present invention is a soap, alkali metal salts of fatty acids, fatty acid hemiester salts, fatty acid protein hydrolyzates, isethionates, lanolin derivatives, aliphatic alcohols, vegetable oils, glycerol, sugars and the like are used as carrier components. It may be, but is not limited thereto. These may be used alone or in combination of two or more thereof.
본 발명의 상기 화장료 조성물은 바람직하게는 두피 모발 케어용 화장료 조성물일 수 있다. 구체적으로 헤어토닉, 헤어크림, 헤어로션, 헤어샴푸, 헤어린스, 헤어컨디셔너, 헤어스프레이, 헤어에어졸, 포마드, 분말, 젤, 헤어팩, 헤어트리트먼트, 눈썹발모제, 속눈썹 발모제, 속눈썹 영양제 등을 예로 들 수 있으나 이에 제한되지 않는다.The cosmetic composition of the present invention may be preferably a cosmetic composition for scalp hair care. Specifically, hair tonic, hair cream, hair lotion, hair shampoo, hair rinse, hair conditioner, hair spray, hair aerosol, pomade, powder, gel, hair pack, hair treatment, eyebrow regrowth, eyelash regrowth, eyelash nutrition But it is not limited thereto.
상기 화학식 1의 화합물 또는 이의 화장품학적으로 허용되는 염은 그 함량이 제한되는 것은 아니나, 화장료 조성물의 총 중량에 대하여 0.001 내지 50 중량%, 바람직하게는 10 중량% 내외로 포함될 수 있다.The compound of Formula 1 or a cosmetically acceptable salt thereof is not limited in content, but may be included in an amount of 0.001 to 50% by weight, preferably 10% by weight, based on the total weight of the cosmetic composition.
식품 조성물Food composition
본 발명은 하기 화학식 1로 표시되는 화합물인 아세톡시차비콜 아세테이트 또는 이의 식품학적으로 허용되는 염을 유효성분으로 포함하는 탈모 방지 또는 발모 촉진용 식품 조성물을 제공한다.The present invention provides a food composition for preventing hair loss or promoting hair growth comprising acetoxychabicol acetate, a compound represented by the following Formula 1, or a food acceptable salt thereof as an active ingredient.
[화학식 1][Formula 1]
본 발명은 또한, 화학식 1로 표시되는 화합물인 아세톡시차비콜 아세테이트 또는 이의 식품학적으로 허용되는 염을 유효성분으로 포함하는 탈모의 예방 또는 개선용 식품 조성물을 제공한다.The present invention also provides a food composition for preventing or improving hair loss comprising acetoxychabicol acetate, a compound represented by the formula (1), or a food acceptable salt thereof as an active ingredient.
본 발명의 화학식 1의 화합물은 천연물로부터 유래되어 안정성이 입증되었으므로 식품 조성물로 사용할 수 있다. 상기 화학식 1의 화합물 또는 이의 식품학적으로 허용되는 염은 그 함량이 제한되는 것은 아니나, 식품 조성물의 총 중량에 대하여 0.001 내지 50 중량%, 바람직하게는 10 중량% 내외로 포함될 수 있다. 또한, 상기 조성물은 식품 조성물에 통상 사용되어 냄새, 맛, 시각 등을 향상시킬 수 있는 추가 성분을 포함할 수 있다. 예들 들어, 비타민 A, C, D, E, B1, B2, B6, B12, 니아신(niacin), 비오틴(biotin), 폴레이트(folate), 판토텐산(panthotenic acid) 등을 포함할 수 있다. 또한, 아연(Zn), 철(Fe), 칼슘(Ca), 크롬(Cr), 마그네슘(Mg), 망간(Mn), 구리(Cu) 등의 미네랄을 포함할 수 있다. 또한, 라이신, 트립토판, 시스테인, 발린 등의 아미노산을 포함할 수 있다. 또한, 방부제(소르빈산 칼륨, 벤조산나트륨, 살리실산, 디히드로초산나트륨 등), 살균제(표백분과 고도 표백분, 차아염소산나트륨 등), 산화방지제(부틸히드록시아니졸(BHA), 부틸히드록시톨루엔(BHT) 등), 착색제(타르색소 등), 발색제(아질산 나트륨, 아초산 나트륨 등), 표백제(아황산나트륨), 조미료(MSG 글루타민산나트륨 등), 감미료(둘신, 사이클레메이트, 사카린, 나트륨 등), 향료(바닐린, 락톤류 등), 팽창제(명반, D-주석산수소칼륨 등), 강화제, 유화제, 증점제(호료), 피막제, 검기초제, 거품억제제, 용제, 개량제 등의 식품 첨가물(food additives)을 첨가할 수 있다. 상기 첨가물은 식품의 종류에 따라 선별되고 적절한 양으로 사용된다.The compound of formula 1 of the present invention can be used as a food composition because it is derived from natural products and has been proven to be stable. The compound of Formula 1 or a food acceptable salt thereof is not limited in content, but may be included in an amount of about 0.001 to 50% by weight, preferably about 10% by weight, based on the total weight of the food composition. In addition, the composition may include additional ingredients that are commonly used in food compositions to improve the smell, taste, time and the like. For example, it may include vitamins A, C, D, E, B1, B2, B6, B12, niacin, biotin, folate, panthotenic acid, and the like. In addition, it may include minerals such as zinc (Zn), iron (Fe), calcium (Ca), chromium (Cr), magnesium (Mg), manganese (Mn), copper (Cu). It may also contain amino acids such as lysine, tryptophan, cysteine, valine and the like. Also preservatives (potassium sorbate, sodium benzoate, salicylic acid, sodium dihydroacetate, etc.), fungicides (bleaching powder and highly bleaching powder, sodium hypochlorite, etc.), antioxidants (butylhydroxyanisol (BHA), butylhydroxytoluene (BHT) ), Colorants (such as tar colors), colorants (such as sodium nitrite, sodium nitrite), bleach (sodium sulfite), seasonings (such as MSG glutamate), sweeteners (ducin, cyclate, saccharin, sodium, etc.), Food additives such as fragrances (vanillin, lactones, etc.), swelling agents (alum, potassium D-tartrate, etc.), reinforcing agents, emulsifiers, thickeners (pigments), coatings, gum herbicides, foam inhibitors, solvents, and improving agents. Can be added. The additive is selected according to the type of food and used in an appropriate amount.
본 발명에서 사용되는 용어, 식품학적으로 허용되는 염은, 양이온과 음이온이 정전기적 인력에 의해 결합하고 있는 물질인 염 중에서도 식품학적으로 사용될 수 있는 형태의 염을 의미하며, 그 종류에 대한 구체적인 예는 상술한 “약학적으로 허용되는 염”의 예를 포함한다.As used herein, the term food acceptable salt means a salt in a form that can be used in food, even among salts in which cations and anions are bound by electrostatic attraction, and specific examples of the types thereof Includes examples of the “pharmaceutically acceptable salts” described above.
본 발명의 식품 조성물에서 화학식 1로 표시되는 화합물의 함량은 사용 목적에 따라 적합하게 결정될 수 있다. 일반적으로, 화학식 1로 표시되는 화합물은 식품 조성물의 총중량에 대하여 0.0001 내지 100 중량%로 첨가될 수 있다.The content of the compound represented by Formula 1 in the food composition of the present invention may be appropriately determined depending on the intended use. In general, the compound represented by Formula 1 may be added at 0.0001 to 100% by weight based on the total weight of the food composition.
본 발명에서, 식품 조성물의 형태에는 특별한 제한이 없으며, 통상적인 의미에서의 식품을 모두 포함한다. 본 발명이 적용될 수 있는 식품으로는, 예를 들어, 음료, 드링크제, 건강기능식품 등이 있다.In the present invention, there is no particular limitation on the form of the food composition, and includes all foods in the usual sense. Foods to which the present invention can be applied include, for example, beverages, drinks, and health functional foods.
본 발명에서 사용되는 용어, 건강기능식품(health functional food)"은 일반식품에 비해 적극적인 건강유지나 증진 효과를 가지는 식품을 의미하고, 건강보조식품(health supplement food)는 건강 보조 목적의 식품을 의미한다. 경우에 따라, 기능성식품, 건강식품, 건강보조식품의 용어는 호용된다. 상기 식품은 유용한 효과를 얻기 위하여 정제, 캅셀, 분말, 과립, 액상, 환 등의 다양한 형태로 제조될 수 있다.As used herein, the term "health functional food" means a food having an active health maintenance or promotion effect compared to a general food, and a health supplement food means a food for health supplement purposes. In some cases, the terms functional food, health food, health supplement food are used in. The food may be prepared in various forms such as tablets, capsules, powders, granules, liquids, pills, etc. in order to obtain useful effects.
본 발명에서 사용되는 용어, 기능식품(functional food)"은 특정보건용 식품(food for special health use, FoSHU)와 동일한 용어로, 영양 공급 외에도 생체조절기능이 효율적으로 나타나도록 가공된 의학, 의료효과가 높은 식품을 의미한다.The term used in the present invention, functional food (functional food) is the same term as a food for special health use (FOSHU), in addition to nutrition, medical, medical effect processed to appear efficiently to regulate the bioregulatory function Means high food.
본 발명의 건강기능식품의 구체적인 예로, 상기 화학식 1의 화합물 또는 이의 식품학적으로 허용되는 염을 이용하여 농산물, 축산물 또는 수산물의 특성을 살려 변형시키는 동시에 저장성을 좋게 한 가공식품을 제조할 수 있다. 상기 건강기능식품은 특별히 이에 제한되지 않으나, 바람직하게는 마아가린, 지방 지속성(fat continuous) 또는 물 지속성(water continuous) 또는 양쪽 지속성(bicontinuous) 스프레드, 지방 감소된 스프레드, 초콜렛, 또는 초콜렛 코팅 또는 초콜렛 속(fillings) 또는 베이커리 속과 같은 과자류, 아이스크림, 아이스크림 코팅, 아이스크림 함유물, 드레싱, 마요네즈, 치즈, 크림 대체물, 건조 스프, 드링크, 시리얼 바, 소스, 스낵바, 유제품, 임상 영양식품, 소아용식품 등의 형태로 제조된 것을 사용할 수 있다.As a specific example of the health functional food of the present invention, by using the compound of Formula 1 or a food-acceptable salt thereof, it is possible to prepare a processed food with improved storage characteristics while modifying the characteristics of agricultural products, animal products or aquatic products. The dietary supplement is not particularly limited, but preferably margarine, fat continuous or water continuous or both continuous spreads, fat reduced spreads, chocolate, or chocolate coating or chocolate loaf. (fillings) or sweets such as bakery, ice cream, ice cream coatings, ice cream ingredients, dressings, mayonnaise, cheese, cream substitutes, dry soups, drinks, cereal bars, sauces, snack bars, dairy products, clinical nutrition foods, pediatric foods It may be used prepared in the form.
본 발명의 화학식 1의 화합물을 유효성분으로 포함하는 탈모 방지 또는 발모 촉진용 조성물은 그 제형을 적절히 변형하여 사람 외의 다른 동물, 특히 애완동물용으로도 사용할 수 있다. Hair loss prevention or hair growth promoting composition comprising the compound of the formula (1) of the present invention as an active ingredient can be used for other animals, especially pets other than humans by appropriately modifying the formulation.
본 발명의 조성물의 용도, 본 발명을 조성물을 이용한 탈모의 예방, 개선 또는 치료방법Use of the composition of the present invention, the method of preventing, ameliorating or treating hair loss using the composition of the present invention
본 발명은 탈모의 예방, 치료 또는 개선, 또는 발모의 촉진을 위한 약제의 제조를 위한, 상술한 약학적 조성물의 용도를 제공한다.The present invention provides the use of the pharmaceutical composition described above for the preparation of a medicament for the prevention, treatment or amelioration of hair loss, or for the promotion of hair growth.
본 발명은 또한 탈모의 예방, 치료 또는 개선, 또는 발모의 촉진을 위한 상술한 약학적, 의약외품, 화장품 또는 식품 조성물의 용도를 제공한다.The present invention also provides the use of the aforementioned pharmaceutical, quasi-drug, cosmetic or food composition for the prevention, treatment or amelioration of hair loss, or the promotion of hair growth.
본 발명은 또한, 탈모의 치료를 필요로 하는 대상체에게, 상술한 약학적을 치료학적으로 유효한 양으로 투여하는 것을 포함하는, 탈모의 치료 방법을 제공한다. 본 발명에서 상기 대상체는 포유류 특히 인간을 포함한다.The present invention also provides a method for treating hair loss, comprising administering to a subject in need thereof a therapeutically effective amount of the above-mentioned pharmaceutical. In the present invention the subject comprises a mammal, in particular a human.
본 발명의 아세톡시차비콜 아세테이트는 모낭의 성장을 촉진하는 효과가 우수하여 탈모를 방지하고 발모를 촉진하는 효과가 탁월할 뿐만 아니라, 천연물로부터 유래된 것으로 부작용이 없어 탈모 방지 또는 발모 촉진용 약학적 조성물, 의약외품 조성물, 화장료 조성물, 그리고 식품 조성물로 다양하게 활용될 수 있다.Acetoxychabicol acetate of the present invention has an excellent effect of promoting the growth of hair follicles to prevent hair loss and promote hair growth, and is derived from natural products and has no side effects, thus preventing hair loss or promoting hair growth. It can be used in various ways as a composition, quasi-drug composition, cosmetic composition, and food composition.
도 1은 본 발명의 아세톡시차비콜 아세테이트의 탈모 방지 및 발모 촉진 효능을 동물 실험을 통해 관찰한 사진이다.1 is a photograph observed through the animal experiments of the hair loss prevention and hair growth promoting effect of the acetoxychabicol acetate of the present invention.
도 2는 사람 모낭 세포 기관 배양에서 본 발명의 아세톡시차비콜 아세테이트의 모낭 성장 촉진 효과를 관찰한 그래프이다.Figure 2 is a graph illustrating the hair follicle growth promoting effect of the acetoxychabicol acetate of the present invention in human hair follicle cell organ culture.
도 3은 대량강(Alpinia galanga) 근경 70% 에탄올 추출물의 HPLC 크로마토그램이다.3 is an HPLC chromatogram of 70% ethanol extract of Alpinia galanga root.
도 4는 대량강 추출물의 탈모 방지 및 발모 촉진 효능을 동물 실험을 통해 관찰한 사진 및 그래프이다.Figure 4 is a photograph and graphs observed through animal experiments to prevent hair loss and hair growth promoting effect of the mass extract.
이하, 본 발명을 실시예를 통하여 보다 상세하게 설명한다. 그러나 이들 실시예는 본 발명을 예시적으로 설명하기 위한 것으로 본 발명의 범위가 이들 실시예에 한정되는 것은 아니다.Hereinafter, the present invention will be described in more detail with reference to Examples. However, these examples are for illustrative purposes only and the scope of the present invention is not limited to these examples.
실시예 1: 아세톡시차비콜 아세테이트의 탈모 방지 및 발모 촉진 효능Example 1 Hair Loss Prevention and Hair Growth Promoting Effect of Acetoxychabicol Acetate
아세톡시차비콜 아세테이트의 탈모 방지 및 발모 촉진 효능을 확인하기 위하여 다음과 같은 동물 실험을 수행하였다. 본 실시예에서 사용한 아세톡시차비콜 아세테이트는 Abcam사로부터 구입하여 사용하였다.In order to confirm the hair loss prevention and hair growth promoting effect of acetoxychabicol acetate, the following animal experiment was performed. Acetoxychabicol acetate used in this example was purchased from Abcam.
7주령의 C57BL/6 마우스 7마리를 3개의 실험군으로 나누어, 3개 실험군 모두 매일 테스토스테론(10 μM 용액, 100 μl 포말)을 마우스 등판 피부에 도포하되, 제1군은 테스토스테론만을 도포하였고, 제2군과 제3군에는 각각 3일차부터는 아세톡시차비콜 아세테이트(10 μM 용액, 50 μl 포말) 또는 미녹시딜(Minoxidil)(2% 용액, 50 μl 포말)을 테스토스테론과 함께 등판 피부에 도포하였다. 상기 실험은 테스토스테론 도포일을 기준으로 17일간 진행되었다.Seven 7-week-old C57BL / 6 mice were divided into three experimental groups, in which all three groups received testosterone (10 μM solution, 100 μl foam) daily on mouse back skin, but the first group applied only testosterone and the second In group 3 and 3, acetoxychabicol acetate (10 μM solution, 50 μl foam) or minoxidil (2% solution, 50 μl foam) was applied to the back skin with testosterone from day 3, respectively. The experiment was conducted for 17 days based on the testosterone application date.
상기 실험 결과, 테스토스테론만 처리한 마우스에서는 점차 탈모가 진행되어 테스토스테론 처리 약 17일차에는 등판 피부에 털이 거의 소실된 것으로 관찰되었다. 이와 달리, 아세톡시차비콜 아세테이트를 도포한 마우스의 경우, 처음에는 다소 털의 소실이 발생하였으나, 테스토스테론만 처리한 마우스에 비하여 털의 밀도가 확연히 높게 유지되었으며, 아세톡시차비콜 아세테이트를 도포한 지 약 14일차에는 털의 밀도가 다시 높아지는 양상을 보였다. 이는 아세톡시차비콜 아세테이트가 테스토스테론에 의한 탈모를 방지하고 동시에 발모를 촉진하는 효능이 있음을 입증하는 것이다(도 1).As a result of the test, hair loss progressed gradually in mice treated only with testosterone, and it was observed that almost 17 days of testosterone treatment showed little hair loss on the back skin. In contrast, in the case of mice coated with acetoxycarbicol acetate, hair loss occurred slightly at first, but the density of hair remained significantly higher than that of the testosterone-treated mice. On the 14th day, the hair density increased again. This demonstrates that acetoxychabicol acetate is effective in preventing hair loss by testosterone and at the same time promoting hair growth (FIG. 1).
아울러, 아세톡시차비콜 아세테이트는 현재 탈모치료제로 사용되고 있는 미녹시딜(MNX)의 효과와 비교하여 유사한 정도의 탈모 방지 및 발모 촉진 효능을 발휘하는 것으로 확인되었다(도 1). 따라서 아세톡시차비콜 아세테이트는 미녹시딜과 유사하거나 그 이상의 탈모 방지 및 발모 촉진 효능을 나타내면서도 천연물 유래로 부작용의 위험이 없어 탈모 치료제로서 보다 다양하게 활용될 수 있을 것으로 기대된다.In addition, acetoxychabicol acetate was confirmed to exhibit a similar degree of hair loss prevention and hair growth promoting effect compared to the effect of minoxidil (MNX) currently used as a hair loss treatment (FIG. 1). Therefore, acetoxychabicol acetate is expected to be used in various ways as a treatment for hair loss because it shows similar or more hair loss prevention and hair growth promoting effects with minoxidil, and there is no risk of side effects derived from natural products.
실시예 2: 아세톡시차비콜 아세테이트의 모낭 성장 촉진 효능Example 2: Hair follicle growth promoting effect of acetoxychabicol acetate
아세톡시차비콜 아세테이트의 모낭 성장 촉진 효능을 확인하기 위하여 다음과 같은 사람 모낭 세포 기관 배양 실험을 수행하였다. 본 실시예에서 사용한 아세톡시차비콜 아세테이트는 Abcam사로부터 구입하여 사용하였다.In order to confirm the hair follicle growth promoting effect of acetoxychabicol acetate, the following human hair follicle cell organ culture experiments were performed. Acetoxychabicol acetate used in this example was purchased from Abcam.
모발이식수술을 받는 환자의 동의를 얻어 두피조직에서 모발을 분리하여 sebaceous gland 아래부분을 정확하게 일자로 자른 다음 아래 부분의 모발을 사용하였다. 조직은 5% CO2와 37℃의 조건아래 100 U penicillin/streptomycin, 10 ng/ml hydrocortisone, 10 ug/ml insulin, 2mM L-glutamin을 첨가한 Williams E 배지에서 유지하며, 500 nM testosterone과 각각의 약물을 농도별로 배지에 처리한 다음 각 조건 마다 9개의 조직을 넣어 배양하였다. 배지는 3일에 한 번씩 바꿔주고 6일 뒤 조직의 자라난 길이를 측정한다. 이러한 사람 모낭세포(n=36)를 4개의 그룹으로 나누어, 제1군은 약물을 처리하지 않은 대조군(control), 제2군은 테스토스테론 500 nM 처리, 제3군은 테스토스테론 500 nM과 아세톡시차비콜 아세테이트 100 nM 처리, 제4군은 테스토스테론 500 nM과 아세톡시차비콜 아세테이트 200 nM을 처리하여 모낭세포에서 자라나는 모발의 길이를 측정하였다. 상기 실험 결과, 테스토스테론만 처리한 실험군에서는 모낭세포 생성되는 모발의 길이가 약 40% 이상의 감소를 보인 반면, 테스토스테론과 아세톡시차비콜 아세테이트를 함께 처리한 실험군에서는 모두 테스토스테론을 처리하지 않은 대조군과 유사한 정도로 모낭세포 생성되는 모발의 길이가 유지되는 것을 확인하였다(도 2). 이는 테스토스테론에 의한 모낭세포 생성되는 발모 억제가 아세톡시차비콜 아세테이트에 의해 회복됨을 입증하는 것이다.With the consent of the patients undergoing hair transplantation, the hair was separated from the scalp tissue, and the lower part of the sebaceous gland was cut to date and used for the lower part of hair. Tissues were maintained in Williams E medium supplemented with 100 U penicillin / streptomycin, 10 ng / ml hydrocortisone, 10 ug / ml insulin and 2 mM L-glutamin under conditions of 5% CO2 and 37 ° C. 500 nM testosterone and each drug Was treated in the medium for each concentration and 9 tissues were added and cultured for each condition. Change the medium every 3 days and measure the length of tissue growth after 6 days. The human hair follicle cells (n = 36) were divided into four groups, the first group was a drug-free control group, the second group was treated with testosterone 500 nM, and the third group was testosterone 500 nM and acetoxychabi. Treatment with 100 nM of call acetate, the fourth group was treated with 500 nM of testosterone and 200 nM of acetoxychabicol acetate to measure hair length growing in hair follicle cells. As a result, the test group treated only with testosterone showed a hair follicle-producing hair of about 40% or more, while the test group treated with testosterone and acetoxychabicol acetate together had a similar degree to the control group without testosterone. It was confirmed that hair follicle generated hair length was maintained (FIG. 2). This demonstrates that hair follicle-producing hair growth inhibition by testosterone is restored by acetoxychabicol acetate.
실시예 3: 아세톡시차비콜 아세테이트를 고농도로 함유하는 대량강 추출물의 제조Example 3: Preparation of Bulk Steel Extract Containing High Concentration of Acetoxychabicol Acetate
시중의 대량강(Alpinia galanga, 태국산)을 이용하여 다음과 같은 방법으로 아세톡시차비콜 아세테이트를 고농도로 함유하는 추출물을 제조하였다.Extracts containing high concentrations of acetoxychabicol acetate were prepared using commercial bulk steels ( Alpinia galanga, Thailand) as follows.
구체적으로, 대량강 근경 생체 50 g을 세절 한 후, 70% 수용성 에탄올을 250 ml 넣고 2시간 동안 초음파 추출을 2회 반복하였다. 상기 방법에 의해 얻어진 추출물을 여과한 후, 여액을 40℃~50℃에서 감압농축한 다음, 동결건조하여 대량강 근경의 70% 에탄올 추출물 2.2g(수율 4.4%)을 수득하였다. 상기 수득된 추출물 중의 아세톡시차비콜 아세테이트 함유량은 14.61%인 것으로 확인되었다(도 3).Specifically, after cutting 50 g of large diameter rhizome biomass, 250 ml of 70% aqueous ethanol was added and the ultrasonic extraction was repeated twice for 2 hours. After filtering the extract obtained by the above method, the filtrate was concentrated under reduced pressure at 40 ℃ ~ 50 ℃, and then lyophilized to obtain 2.2 g (yield 4.4%) of 70% ethanol extract of the mass root diameter. The acetoxychabicol acetate content in the obtained extract was found to be 14.61% (FIG. 3).
실시예 4: 대량강 추출물의 탈모 방지 및 발모 촉진 효능Example 4: Hair loss prevention and hair growth promoting effect of the mass extract
상기 실시예 3에서 제조한 대량강 추출물을 이용하여 다음과 같은 동물실험을 수행하였다.Animal experiments were performed using the bulk steel extract prepared in Example 3 as follows.
8주령의 C57BL/6 마우스 2마리의 등판 털을 모두 제거한 다음, 2개의 실험군으로 나누어 2개 실험군 모두 매일 테스토스테론(2mg/ml 용액, 100 μl 포말)을 마우스 등판 피부에 도포하되, 제1군은 테스토스테론만을 도포하였고, 제2군은 실시예 3에서 제조한 대량강 추출물을 테스토스테론과 함께 등판 피부에 도포하였다. 상기 실험은 테스토스테론 도포일을 기준으로 7일간 진행되었다. 7일 후 마우스 등판 피부 털의 상태 및 모낭 크기를 측정하였다.Remove all dorsal hairs from two 8-week-old C57BL / 6 mice, divide them into two groups, and apply testosterone (2 mg / ml solution, 100 μl foam) to the back of the mouse daily in both groups. Only testosterone was applied, and the second group applied the bulk steel extract prepared in Example 3 to the back skin along with testosterone. The experiment was conducted for 7 days based on the testosterone application date. After 7 days the condition and hair follicle size of the mouse back skin hair were measured.
상기 실험 결과, 테스토스테론만 도포한 경우에는 마우스 등판 피부의 털이 거의 소실된 반면, 대량강 추출물을 함께 도포한 마우스의 경우 털이 소실되었던 등판 피부에 털의 성장이 촉진되어 털의 밀도가 높아진 것으로 확인되었다. 아울러, 모낭의 크기 또한 테스토스테론만 도포한 경우와 비교하여 월등한 성장을 나타내어 아세톡시차비콜 아세테이트가 고농도로 함유된 대량강 추출물의 탈모 방지 및 발모 촉진 효능을 확인할 수 있었다(도 4).As a result of the test, only testosterone was almost lost to the hair of the back of the mouse, whereas in the case of mice coated with a mass river extract, hair growth was promoted on the back of the hair which had been lost, thereby increasing the hair density. . In addition, the size of the hair follicles also showed superior growth compared to the case of applying only testosterone, confirming the hair loss prevention and hair growth promoting effect of the bulk steel extract containing high concentration of acetoxychabicol acetate (FIG. 4).
본 명세서는 본 발명의 기술 분야에서 통상의 지식을 가진 자이면 충분히 인식하고 유추할 수 있는 내용은 그 상세한 기재를 생략하였으며, 본 명세서에 기재된 구체적인 예시들 이외에 본 발명의 기술적 사상이나 필수적 구성을 변경하지 않는 범위 내에서 보다 다양한 변형이 가능하다. 따라서 본 발명은 본 명세서에서 구체적으로 설명하고 예시한 것과 다른 방식으로도 실시될 수 있으며, 이는 본 발명의 기술 분야에 통상의 지식을 가진 자이면 이해할 수 있는 사항이다.In the present specification, those skilled in the art of the present invention can fully recognize and infer the details that have been omitted, and the technical spirit or essential configuration of the present invention in addition to the specific examples described in this specification are changed. Many more variations are possible without departing. Therefore, the present invention may be implemented in a manner different from that specifically described and illustrated herein, which can be understood by those skilled in the art.
Claims (10)
- 하기 화학식 1로 표시되는 화합물 또는 이의 약학적으로 허용되는 염을 유효성분으로 포함하는 탈모 방지 또는 발모 촉진용 약학적 조성물.A pharmaceutical composition for preventing hair loss or promoting hair growth comprising a compound represented by the following Formula 1 or a pharmaceutically acceptable salt thereof as an active ingredient.[화학식 1][Formula 1]
- 제1항에 있어서, 상기 조성물은 모낭의 성장을 촉진하는 효능을 갖는 것인 약학적 조성물.The pharmaceutical composition of claim 1, wherein the composition has an effect of promoting hair follicle growth.
- 제3항에 있어서, 상기 조성물은 모낭의 성장을 촉진하는 효능을 갖는 것인 의약외품 조성물.The quasi-drug composition according to claim 3, wherein the composition has an effect of promoting hair follicle growth.
- 제5항에 있어서, 상기 조성물은 모낭의 성장을 촉진하는 효능을 갖는 것인 화장료 조성물.The cosmetic composition according to claim 5, wherein the composition has an effect of promoting the growth of hair follicles.
- 제7항에 있어서, 상기 식품 조성물은 모낭의 성장을 촉진하는 효능을 갖는 것인 식품 조성물.The food composition of claim 7, wherein the food composition has an effect of promoting the growth of hair follicles.
- 탈모의 예방, 치료 또는 개선을 위한 약제의 제조를 위한, 제1항에 따른 약학적 조성물의 용도를 제공한다.The use of a pharmaceutical composition according to claim 1 for the manufacture of a medicament for the prevention, treatment or amelioration of hair loss is provided.
- 탈모의 치료를 필요로 하는 대상체에게, 제1항에 따른 약학적 조성물을 치료학적으로 유효한 양으로 투여하는 것을 포함하는, 탈모의 치료 방법. A method of treating hair loss comprising administering to a subject in need thereof a pharmaceutical composition in accordance with claim 1 in a therapeutically effective amount.
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US5192534A (en) * | 1988-12-30 | 1993-03-09 | L'oreal | Composition for inducing and stimulating hair growth and/or retarding its loss, based on pyrimidine derivatives and sunscreens |
US5258391A (en) * | 1987-05-15 | 1993-11-02 | Scott Eugene J Van | Phenyl alpha acyloxyalkanoic acids, derivatives and their therapeutic use |
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US20150231045A1 (en) * | 2012-09-07 | 2015-08-20 | Analyticon Discovery Gmbh | Anti-dandruff composition comprising 1-acetoxychavicol acetate |
US20170015700A1 (en) * | 2014-03-10 | 2017-01-19 | Giuliani S.P.A. | Compounds with a combined antioxidant activity against free radicals together with an anti-inflammatory action, and pharmaceutical and cosmetic compositions containing them for the treatment of skin and hair |
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US5258391A (en) * | 1987-05-15 | 1993-11-02 | Scott Eugene J Van | Phenyl alpha acyloxyalkanoic acids, derivatives and their therapeutic use |
US5567702A (en) * | 1987-08-12 | 1996-10-22 | L'oreal | Combination of pyrimidine derivatives and retinoids, as separate components, for inducing and stimulating hair growth and reducing its loss |
US5192534A (en) * | 1988-12-30 | 1993-03-09 | L'oreal | Composition for inducing and stimulating hair growth and/or retarding its loss, based on pyrimidine derivatives and sunscreens |
US20150231045A1 (en) * | 2012-09-07 | 2015-08-20 | Analyticon Discovery Gmbh | Anti-dandruff composition comprising 1-acetoxychavicol acetate |
US20170015700A1 (en) * | 2014-03-10 | 2017-01-19 | Giuliani S.P.A. | Compounds with a combined antioxidant activity against free radicals together with an anti-inflammatory action, and pharmaceutical and cosmetic compositions containing them for the treatment of skin and hair |
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